1211757-82-2

Upstream product

• 28987-46-4 4-fluoro-1-nitro-2-(propan-2-yloxy)benzene 
• 832113-96-9 methyl 4-chloro-5-methylthieno[2,3-d]pyrimidine-6-carboxylate 
• 148583-65-7 4-Fluoro-2-methylethoxyaniline 

Downstream Products

• 1211757-83-3 4-((4-fluoro-2-isopropoxyphenyl)amino)-5-methylthieno[2,3-d]pyrimidine-6-carboxylic acid 

Relevant academic research and scientific papers

An integrated approach for discovery of highly potent and selective Mnk inhibitors: Screening, synthesis and SAR analysis

Deregulation of protein synthesis is a common event in cancer. As MAPK-interacting kinases (Mnks) play critical roles in regulation of protein synthesis, they have emerged as novel anti-cancer targets. Mnks phosphorylate eukaryotic initiation factor 4E (eIF4E) and promote eIF4E-mediated oncogenic activity. Given that the kinase activity of Mnks is essential for oncogenesis but is dispensable for normal development, the discovery of potent and selective pharmacological Mnk inhibitors provides pharmacological target validation and offers a new strategy for cancer treatment. Herein, comprehensive in silico screening approaches were deployed, and three thieno[2,3-d]pyrimidine and pyrazolo[3,4-d]pyrimidine derivatives were identified as hit compounds. Further chemical modification of thieno[2,3-d]pyrimidine derivative 3 has given rise to a series of highly potent Mnk2 inhibitors that could be potential leads for the treatment of acute myeloid leukemia.

Design, synthesis and activity of Mnk1 and Mnk2 selective inhibitors containing thieno[2,3-d]pyrimidine scaffold

The mitogen-activated protein kinase-interacting kinases 1 and 2 (MNK1 and MNK2) phosphorylate eukaryotic initiation factor 4E (eIF4E) and play important roles in promoting tumorigenesis and metabolic disease. Thus, inhibiting these enzymes might be valua

THIENOPYRIMIDINES CONTAINING A SUBSTITUTED ALKYL GROUP FOR PHARMACEUTICAL COMPOSITIONS

The present invention relates to novel thienopyhmidine compounds of general formula pharmaceutical compositions comprising these compounds and their therapeutic use for the prophylaxis and/or treatment of diseases which can be influenced by the inhibition of the kinase activity of Mnk1 and/or Mnk2 (Mnk2a or Mnk2b) and/or variants thereof.

THIENOPYRIMIDINES CONTAINING A SUBSTITUTED ALKYL GROUP FOR PHARMACEUTICAL COMPOSITIONS

The present invention relates to novel thienopyrimidine compounds of general formula pharmaceutical compositions comprising these compounds and their therapeutic use for the prophylaxis and/or treatment of diseases which can be influenced by the inhibition of the kinase activity of Mnk1 and/or Mnk2 (Mnk2a or Mnk2b) and/or variants thereof.

THIENOPYRIMIDINES FOR PHARMACEUTICAL COMPOSITIONS

The present invention relates to novel pharmaceutical compositions comprising thienopyrimidine compounds according to formula (I). Moreover, the present invention relates to the use of the thienopyrimidine compounds of the invention for the production of